TEZOSENTAN
| 中文名称 | TEZOSENTAN |
|---|---|
| 中文同义词 | 化合物 T17064 |
| 英文名称 | TEZOSENTAN |
| 英文同义词 | TEZOSENTAN;N-[6-(2-Hydroxyethoxy)-5-(2-Methoxyphenoxy)-2-[2-(2H-tetrazol-5-yl)-4-pyridinyl]-4-pyriMidinyl]-5-(1-Methylethyl)-2-pyridinesulfonaMide;N-(2-(2-(2H-Tetrazol-5-yl)pyridin-4-yl)-6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)pyrimidin-4-yl)-5;N-(2-(2-(2H-Tetrazol-5-yl)pyridin-4-yl)-6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)pyrimidin-4-yl;N-(2-(2-(2H-Tetrazol-5-yl)pyridin-4-yl)-6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)pyrimidin-4-yl)-5-isopropylpyridine-2-sulfonamide;RO 610612;2-Pyridinesulfonamide, N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-[2-(2H-tetrazol-5-yl)-4-pyridinyl]-4-pyrimidinyl]-5-(1-methylethyl)- |
| CAS号 | 180384-57-0 |
| 分子式 | C27H27N9O6S |
| 分子量 | 605.62 |
| EINECS号 | |
| 相关类别 | Aromatics;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Sulfur & Selenium Compounds |
| Mol文件 | 180384-57-0.mol |
| 结构式 |  |
TEZOSENTAN 性质
| 熔点 | 198-200° |
|---|---|
| 沸点 | 761.2±70.0 °C(Predicted) |
| 密度 | 1.432±0.06 g/cm3(Predicted) |
| 储存条件 | 2-8°C |
| 溶解度 | 溶于二甲基亚砜 |
| 酸度系数(pKa) | 2.93±0.10(Predicted) |
| 形态 | 固体 |
| 颜色 | 米白色至灰色 |
|
ET A 9.5 (pA2) |
ET B 7.7 (pA2) |
Affinity of Tezosentan for the ET receptors is assessed in different cells and tissues. Tezosentan inhibits the specific 125 I-labeled ET-1 binding to ETA receptors with an inhibitory potency (K i ) of 0.3 nM on CHO cells and of 18 nM on membranes of baculovirus-infected insect cells. Similarly, Tezosentan inhibits the specific binding of 125 I-labeled ET-1, ET-3, or sarafotoxin S6c to ET B receptors with an inhibitory affinity of 10 to 21 nM. Tezosentan up to a concentration of 1 μM did not exhibit any binding inhibitory activity in 27 radioligand binding assays different from ET binding. On H1 central, 5-hydroxytryptamine2A, and vasopressin V1 receptors, Tezosentan (1 μM) induces a weak inhibition of less than 20%.
In pithed Wistar rats, Tezosentan dose-dependently inhibits the pressor effect of big ET-1 (P<0.001 at all doses). At the lowest dose tested of 1 mg/kg, Tezosentan inhibits the pressor effect of the various doses of big ET-1 by 50 to 80%. Tezosentan has no effect by itself on blood pressure in these pithed rats. Tezosentan is very effective in a rat model of acute renal failure. ET antagonists have been shown to prevent the vasoconstriction and the renal failure that follow acute renal ischemia in rats.